Discovery of a small molecule insulin mimetic with antidiabetic activity in mice.
Science
; 284(5416): 974-7, 1999 May 07.
Article
en En
| MEDLINE
| ID: mdl-10320380
ABSTRACT
Insulin elicits a spectrum of biological responses by binding to its cell surface receptor. In a screen for small molecules that activate the human insulin receptor tyrosine kinase, a nonpeptidyl fungal metabolite (L-783,281) was identified that acted as an insulin mimetic in several biochemical and cellular assays. The compound was selective for insulin receptor versus insulin-like growth factor I (IGFI) receptor and other receptor tyrosine kinases. Oral administration of L-783,281 to two mouse models of diabetes resulted in significant lowering in blood glucose levels. These results demonstrate the feasibility of discovering novel insulin receptor activators that may lead to new therapies for diabetes.
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Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Ascomicetos
/
Receptor de Insulina
/
Diabetes Mellitus Tipo 2
/
Hipoglucemiantes
/
Indoles
/
Insulina
Tipo de estudio:
Prognostic_studies
Idioma:
En
Revista:
Science
Año:
1999
Tipo del documento:
Article
País de afiliación:
Estados Unidos